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Generated: December 16, 2017

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Claims for Patent: 5,965,168

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Claims for Patent: 5,965,168

Title: Microencapsulated 3-piperidinyl-substituted 1,2-benzisoxazoles and 1,2-benzisothiazoles
Abstract:The invention relates to a pharmaceutical composition comprising a biodegradable and biocompatible microparticle composition comprising a 1,2-benzazole of the formula ##STR1## and the pharmaceutically acceptable acid addition salts thereof, within a polymeric matrix.
Inventor(s): Mesens; Jean (Wechelderzande, BE), Rickey; Michael E. (Loveland, OH), Atkins; Thomas J. (York, PA)
Assignee: Alkermes Controlled Therapeutics, Inc. II (Cambridge, MA) Janssen Pharmaceutica (BE)
Application Number:09/005,549
Patent Claims: 1. A sustained-release microparticle comprising: a 1,2-benzazole of the formula ##STR16## and the pharmaceutically acceptable acid addition salts thereof, wherein R is hydrogen or alkyl of 1 to 6 carbon atoms;

R.sup.1 and R.sup.2 are independently selected from the group consisting of hydrogen, halo, hydroxy, alkyloxy of 1 to 6 carbon atoms, and C alkyl of 1 to 6 carbon atoms;

X is O or S;

Alk is C.sub.1-4 alkanediyl; and

Q is a radical of formula ##STR17## wherein R.sup.3 is hydrogen or alkyl of 1 to 6 carbon atoms;

Z is --S--, --CH.sub.2 --, or --CR.sup.4 .dbd.CR.sup.5 --; where R.sup.4 and R.sup.5 are independently selected from the group consisting of hydrogen or alkyl of 1 to 6 carbon atoms;

A is a bivalent radical --CH.sub.2 --CH.sub.2 --, --CH.sub.2 --CH.sub.2 --CH.sub.2 -- or CR.sup.6 .dbd.CR.sup.7 --;

where R.sup.6 and R.sup.7 are independently selected from the group consisting of hydrogen, halo, amino or alkyl of 1 to 6 carbon atoms; and

R.sup.8 is hydrogen or hydroxyl; and a biodegradable and biocompatible polymeric matrix.

2. The sustained-release microparticle of claim 1, wherein the biodegradable and biocompatible polymeric matrix is selected from the group consisting of poly(glycolic acid), poly-D,L-lactic acid, poly-L-lactic acid, copolymers of the foregoing, poly(aliphatic carboxylic acids), copolyoxalates, polycaprolactone, polydioxonone, poly(ortho carbonates), poly(acetals), poly(lactic acid-caprolactone), polyorthoesters, poly(glycolic acid-caprolactone), polyanhydrides, albumin, casein, and waxes.

3. The sustained-release microparticle of claim 1, wherein said 1,2-benzazole comprises 1 to 90 wt. % of the microparticle.

4. The sustained-release microparticle of claim 1, wherein said 1,2-benzazole comprises about 35 to 40 wt. % of the microparticle.

5. The sustained-release microparticle of claim 1, wherein the microparticle ranges in size from 1 to 500 microns.

6. The sustained-release microparticle of claim 1, wherein the microparticle ranges in size from 25 to 180 microns.

7. The sustained-release microparticle of claim 1, wherein the microparticle is formulated in a liquid injection vehicle.

8. The sustained-release microparticle of claim 7, wherein said liquid injection vehicle is selected from the group consisting of

A. physiological saline solution and

B. an aqueous solution of carboxymethyl cellulose with a surfactant.

9. The sustained-release microparticle of claim 1, wherein the microparticle is administered by intramuscular injection.

10. The sustained-release microparticle of claim 1, wherein the microparticle is administered by subcutaneous injection.

11. The sustained-release microparticle of claim 1, wherein the 1,2-benzazole is selected from the group consisting of 3-[2-[4-(6-fluoro-1,2-benzisoxazol-3-yl)-1-piperidinyl)ethyl]-6,7,8,9-tetr ahydro-2-methyl-4H-pyrido[1,2-a]pyrimidin-4-one and the pharmaceutically acceptable acid addition salts thereof.

12. The sustained-release microparticle of claim 1, wherein the 1,2-benzazole is selected from the group consisting of 3-[2-[4-(6-fluoro-1,2-benzisoxazol-3-yl)-1-piperidinyl)ethyl]-6,7,8,9-tetr ahydro-9-hydroxy-2-methyl-4H-pyrido[1,2-a]pyrimidin-4-one and the pharmaceutically acceptable acid addition salts thereof.
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